Ramipril



Better Known as: Altace or Ramipro

 * Marketed By: King Pharmaceuticals (Now part of Pfizer Inc.)


 * Major Indication: Hypertension & Congestive Heart Failure


 * Drug Class: ACE Inhibitor
 * Date of FDA Approval (Patent Expiration): 1991 (2007)


 * 2006 Sales: $650 Million
 * Importance: One of the best selling Angiotensin-Converting Enzyme Inhibitors of all time. Long acting ACE Inhibitor.
 * See Pharmaceutical Drugs for more information about other drugs and diseases

Mechanism of Action
Angiotensin II has been implicated in cardiac, renal and vascular diseases. Bradykinin, a small peptide that counterbalance the effects of Angiotensin II by acting as a strong vasodilator upon binding AT2, is degraded by the same ACE-1 enzyme. Since ACE-1 is the primary producer of Angiotensin II and degrader of Bradykinins, inhibition of ACE-1 has proven an effective treatment for Hypertension and Congestive Heart Failure. Ramipril is quickly metabolized into Ramiprilat, the most active metabolite of Ramipril. Ramiprilat binds to the active site of Angiotensin-Converting Enzyme, actively inhibiting ACE-1 from binding and converting Angiotensin I into Angiotensin II. ACE-1  binds Ramiprilat using residues Glu 395, His 497, Lys 495, Gln 265, Tyr 504, Tyr 496 and Tyr 507, tightly affixing the inhibitor to the active site of ACE-1.